Improving Physicochemical Properties of Repaglinide Through Pharmaceutical Adduct Formation

Background: Many formulation strategies are presently in development in pharmaceutical industry. However, the formation of pharmaceutical adducts is considered to be the most appropriate technique for improving the drug solubility and dissolution as no chemical bond changes are involved in this technique.Purpose: This technique is highly used for compounds which are not able to give viable formulation products with standard techniques such as salt formation and polymorph generation. In the present study, this method is applied to repaglinide, which is an hypoglycemic agent, with compromised solubility. Methods: The adducts were prepared by slow evaporation method and characterized using DSC, FTIR and PXRD studies. The solubility and dissolution studies were carried out to determine the increased solubility of drug in adducts. The drug amount interacted with coformers has also been determined. Results: The present study demonstrates the improvement in solubility and thus dissolution of repaglinide in adducts.Conclusion: The adducts formed in the present study can be further exploited to prepare formulation of repaglinide adducts with better physicochemical characteristics

A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold

Background: Benzimidazole is a category of heterocyclic aromatic compounds formed from the fusion of six membered benzene with five membered imidazolering. The moiety possesses diverse biological and clinical applications. A number of studies have shown that a varied substituent around the benzimidazole nucleus results in pharmacologically active compounds of therapeutic interest. Purpose: Owing to its number of pharmacological properties, this moiety is of choice of interest in designing and synthesis of new therapeutic compounds. The existence of the benzimidazole core in numerous groups of biological agents like antimicrobial, antiviral, antiparasitic, antihypertensive, anticancer, CNS stimulant as well as depressants has made important scaffold for development of many newer therapeutic agents. There is utmost need to understand the synthesis and associated role of benzimidazole derived compounds in different diseases. Therefore, in the present review, we attempt to discuss various derivatives of benzimidazole nucleus with different pharmacological activities. Conclusion: Benzimidazoles have played a great role in discovery of drug and development. Huge attempt has been made towards benzimidazole heterocyclic-based organic compounds with great excellence that resulted in drugs with enormous biological activity. Therapeutic drugs containing benzimidazole nucleus are used in building drugs that serve to be an active area of research. This article becomes a source that will lead to discovery of new opportunities for all researchers interested in benzimidazole-based heterocyclic medicinal chemistry

Ranitidine Induced Hepatotoxicity: A Review

Background: Ranitidine (RAN) is one of the common drugs associated with idiosyncratic adverse drug reactions (IADRs) in humans. It was found to be associated with severe adverse drug reactions due to the presence of contaminants such as N-Nitrosodimethylamine (NDMA) which is claimed to be carcinogenic. As a consequence, on April 1, 2020, United States Food and Drug Administration (USFDA) had decided to call off all the RAN products from the market. The exact cause of RAN associated idiosyncratic hepatotoxicity is not clear yet. Purpose: To summarize and analyze the reason behind the withdrawal of RAN products from the market and whether ranitidine will be available again in future or will FDA withdraw approvals of ranitidine National Drug Authority (NDA) and an abbreviated new drug application (ANDA)? Methods: We performed a systematic PubMed/MEDLINE search of studies investigating the reason behind the withdrawal of RAN products and explored the possible mechanism associated with RAN induced hepatotoxicity.Conclusion: RAN induced liver injury is difficult to diagnose and study because of its relative rarity and unpredictive occurrence. Recent studies suggest that most of the RAN associated idiosyncratic reactions may lead to hepatocyte damage, followed by a series of events, such as activation of specific T- and B-cells, release of proinflammatory mediators like TNFα, interleukins, various cytokines and chemokines. The exact cause of RAN associated idiosyncratic hepatotoxicity is not clear yet. More studies must be carried out on this to know about the exact reason behind RAN associated hepatotoxicity

Pharmaceutical Applications of Xanthan Gum in Ophthalmic Delivery Systems

Introduction: Ophthalmic delivery system is one of the challenging domains of formulation and development due to tear dilutions, drug loss due to lacrimal drainage, limited volume and pre-corneal barriers. Several pharmaceutical technologies are exploited in order to counter the challenges posed by ocular route such as emulsions and suspensions. But all these technologies have stability issues which lead to their limited use.Background: Among polysaccharides, xanthan gum, a natural occurring biodegradable exopolysaccharide extracted from bacterium Xanthomonas campestris is widely accepted as one of the potential polysaccharide in ophthalmic delivery systems.Review Results: Xanthan gum is commonly used as an additive to various ophthalmic formulations due to its mucoadhesive property and imparting stability to various novel pharmaceutical technologies for ophthalmic. Xanthan gum also allows chemical modifications with various ligands which consequently allow controlled release, modified dissolution rate and viscoelasticity. Conclusion: In this review we are providing an insight over potential of pharmaceutical applications of xanthan gum. Also, we have discussed the scope of chemical modifications in xanthan gum with modified physicochemical properties

Antioxidant Potential of Glycyrrhiza glabra L. roots: In-Vitro Evidences

Background: The study was aimed to determine the mechanism of antioxidant effects of Glycyrrhiza glabra L. (GG) roots using in-vitro assays.Methods: The various extracts of GG roots were prepared and evaluated for DPPH scavenging, reducing effects and nitric oxide inhibiting activities. Prepared extracts were screened for the presence of various phytochemicals and quantified on the basis of phytochemical present therein.Results: The results showed that all the prepared extracts contained phenolic compounds. Also, extract showed appreciable antioxidant effects in all three assays employed. However, among prepared extracts, ethylacetate extract was found to have strong free radical inhibition, ferric reducing potential and nitric oxide inhibitory effects. The reason for high antioxidant activity in ethylacetate extract could be attributed to the significant amount of phenol compounds present in it. Conclusion: Evidently, GG’s capacity to scavenge free radicals, reducing potential and inhibit nitric oxide contributes to its antioxidant effects and thus, could be a strong candidate for developing antioxidant based drug therapy

Phytoalexins: Sources and Their Pharmacological Potential

Background: Plants are easily prone towards microbial infections on exposure to microorganisms and pathogens. In order to defense, plants produce low molecular weight secondary metabolites which were later known as “Phytoalexins”. These molecules have vast therapeutic potential also. Purpose: The purpose of this review is to explore the phytoalexins and their pharmacological effects.Methods: The data included from the articles were published from Web of Science, PubMed, Medline, Scopus, and Embase by using relevant keywords including plants possessing phytoalexins and their specific biological applications.Results: The review insights the potential of phytoalexins in various diseases and to explore phytoalexins applications in human health and disease control. Conclusions: On the basis of this review it may be concluded that phytoalexins have tremendous potential in the treatment and prevention of various life-threatening diseases like diabetes mellitus, cancer, brain damage, and heart attack

The Effect of Modification Methods on the Properties of Lentinus Tuber Regium Powders

The current work considered the influence of methods of modification on the physical characteristics of Lentinus Tuber Regium (LTR) powders. The sclerotia of the LTR was pulverized to 250.0 μm and coded as native Lentinus Tuber Regium (NLTR-A). A 500.0 g of NLTR-A was submerged in 3.5 % w/v sodium hypochlorite and stirred continuously for 30.0 min. The resultant slurry was washed severally with purified water until it was neutral to litmus. The mass was dried in an oven at 60.0 °C for 2.0 h, pulverized (250.0 μm) and was noted as the modified Lentinus Tuber Regiumpowder (MLTR-B). Another 500.0 g of NLTR-A was extracted with 70.0 % v/v ethanol in a Soxhlet extractor. The resultant powder was dried at 60.0 o C for 2.0 h, micronized (250.0 μm) and coded as the modified Lentinus Tuber Regium powder (MLTR-C). Additional 500.0 g of NLTR-A was submerged in 600.0 mL of 0.5 N sodium hydroxide in a 1.0 L beaker and shaken constantly for 30.0 min. The subsequent material was splashed with purified water until the material was neutral to litmus. The mass was freed from water and introduced into 200.0 mL of 0.5 N hydrochloric acid. It was agitated for 30.0 min in a water bath at 100.0 °C. It was flooded in purified water until it was neutral to litmus. The product was dried to constant weight at 60.0 °C and pulverized (250.0 μm). The product was coded as the modified Lentinus Tuber Regium powder (MLTR-D). Generally, NLTR-A, MLTR-B, MLTR-C and MLTR-D were investigated for their organoleptic, solubility, pH, moisture studies, scanning electron microscopy (SEM), x-ray diffractometry (XRD), flow parameters and densities. The results showed that both the native and the modified powders were insoluble in water and most organic solvents. The pH of the derived powders was consistently higher. SEM and XRD revealed morphological differences in each of the derived powders, though, all the powders were non-crystalline. The respective modification methods brought about an improvement in the hydrophilic and flow properties of the modified powders when compared to the native form of LT

UV-Spectrophotometry - Multicomponent Mode of Analysis for Simultaneous Estimation of Brinzolamide and Brimonidine Tartrate in Bulk and Ophthalmic Formulation

Brinzolamide (BRZ) and Brimonidine Tartrate (BT) in combination are available as an ophthalmic suspension in the ratio of 5:1. A simple, reproducible and efficient method for the simultaneous determination of BRZ and BT in Bulk and Ophthalmic formulation has been developed. The absorbance was assessed at two wavelengths i.e. 252.40 nm (λ max of BRZ) and 246 nm (λmax of BT) in methanol. In this method, BRZ and BT executed linearity in the concentration range of 5-35 μg/mL and 3-18 μg/mL, respectively at their respective λ max. The developed method was found to be accurate, precise and rugged as marked by small values of % RSD according to ICH guidelines

Evaluation of Antimitotic Activity of Momordica Dioica Fruits on Allium Cepa Root Meristamatic Cells

Natural occurring phenolic compounds play an important role in cancer prevention and shows antimitotic activity. Number of active constituents like phenolic acid, curcuminoids, coumarine, ligans, quinones, etc. is showing antimitotic activity of Momordica dioica. The present work is on phytochemical investigation and examines antimitotic activity of aqueous extract of fruits Momordica dioica at concentration of 15 mg/ml on Allium cepa root meristamatic cells.The fruits are air dried and extracted with solvents like water by maceration method. The evaluation of antimitotic activity is done by using Allium cepa root meristamatic cells parameters where and methotrexate was used as a standard drugs. In Allium assay, aqueous extract of fruits of Momordica diocia (15 mg/ml) and methotrexate act against cells of allium roots and lesser the growth of root and mitotic index when compared with distilled water as control group. The result indicated that cytotoxic property is due to presence of phenolic, alkaloids and flavonoids compounds in 15 mg/ml concentration of aqueous extract of Momordica diocia fruits extract.On the basis of result, we concluded that, 15 mg/ml concentration of Momordica dioica fruits shows good antimitotic activity on the Allium cepa root tip assay

UV Method Development and Validation of Ellagic Acid for its Rapid Quantitative Estimation

Development and validation of a simple UV- Spectroscopy method was done for the quantitative analysis of Ellagic Acid (EA). The stock solution of 50μg/ml was prepared and scanned, for which absorption maxima was found to be 277nm. Further dilutions to different concentrations (1-5μg/ml) were prepared and analyzed at 277nm. The method so developed was validated as per ICH guidelines for: linearity, robustness, precision, accuracy, limit of detection and quantification. The Lambert- Beer’s law is followed in the range (1-5μg/ml) with correlation coefficient value 0.9994. It was observed that the method is precise and accurate for EA analysis with good recovery percent of 94.47% to 106.83%. The method developed was further employed for determining the entrapment efficiency of ellagic acid and its release from its nanoparticle dosage form. The method may be utilized for determining the concentration of EA when present as formulation and in combination with other drugs